Autonomic Pharm & Kinetics Flashcards
On the log enzyme kinetics graph, y-intercept is equal to?
1/Vmax
The lower the Km,
the _____ the affinity.
higher
On the log kinetics graph:
Competitive inhibitors cross each other competitively.
T/F
T
They all cross on 1/Vmax
On the log kinetics graph:
Noncompetitive inhibitors do not cross each other.
T/F
T
they have different Km’s
Vd = ?
amt of drug in body /
plasma drug concentration
t1/2 = ?
0.7 * Vd / clearanc
A drug infused at a constant rate reaches about 94% of steady state after x half-lives?
x = 4
Loading dose = ?
Cp * Vd/F
Cp = target plasma conc. F = bioavailability: =1 per IV
Phase 1 metabolism involves?
yields?
reduction, oxidation, hydrolysis
cytochrome P450
yields slightly polar, still-active water-soluble metabolites
Geriatrics lost this first
Phase 2 metabolism involves?
yields?
acetylation, glucuronidation, sulfation, conjugation
yields very polar, inactive metabolites
Potency = ? Efficacy = ?
Potency = amt needed for a given effect
Efficacy = maximal effect
Therapeutic index =
TD50 /
ED50
(median toxic dose /
median effective dose)
Skeletal Muscle.
N or M?
neurotransmitter?
N
ACh
PNS: Cardiac & Smooth Muscle, gland cells.
N or M?
neurotransmitter?
N——-M (2 neurons)
Ach Ach
All sympathetic @ ganglion.
N or M?
neurotransmitter?
N
ACh
Sympathetic 2nd neuron @ sweat glands:
N or M?
neurotransmitter?
M
ACh
Sympathetic @ cardiac and smooth muscle, gland cells, nerve terminals
neurotransmitter?
NE @ alpha or beta
Sympathetic at Renal vascular smooth muscle
receptor??
D1
Sympathetic @ adrenal medulla
N or M?
neurotransmitter?
N, ACh
G-protein-linked 2nd messengers:
a1 ->
G-prot class?
functions?
q
Inc’d vascular smooth muscle contraction
G-protein-linked 2nd messengers:
a2
i Dec'd sympathetic outflow Dec'd insulin release Dec'd lipolysis Inc'd platelet aggregation
G-protein-linked 2nd messengers:
B1
s Inc'd HR, Inc'd contactility Inc'd renin release Inc'd lipolysis
G-protein-linked 2nd messengers:
B2
s vasodilation, bronchodilation Inc'd HR, contractility, lipolysis, insulin release, aqueous humor production Dec'd uterine tone (tocolysis) Ciliary muscle relaxation
G-protein-linked 2nd messengers:
M1
q
CNS
G-protein-linked 2nd messengers:
M2
i
Dec’d HR & contractility of atria
G-protein-linked 2nd messengers:
M3
q
Inc’d exocrine gland secretions, gut peristalsis, bladder contraction, bronchoconstriction, pupillary sphincter muscle (miosis) & ciliary muscle contraction (accommodation)
G-protein-linked 2nd messengers:
D1
s
relaxes renal vascular smooth muscle
G-protein-linked 2nd messengers:
D2
i
modulates transmitter release, esp in brain
G-protein-linked 2nd messengers:
H1
q Inc'd nasal/bronchial mucus bronchconstriction pruritis pain